公开(公告)号：US20160257685A1

公开(公告)日：2016-09-08

申请号：US15156887

申请日：2016-05-17

申请人： University of Kansas ,  The Scripps Research Institute

发明人： Jeffrey Aube ,  Laura Bohn ,  Thomas Edward Prisinzano ,  Frank John Schoenen ,  Kevin J. Frankowski

IPC分类号： C07D471/14 ,  C07D401/14 ,  C07D409/14 ,  C07D401/04 ,  C07D471/04 ,  C07D405/14

CPC分类号： C07D471/14 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4985 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.

摘要翻译： 本发明是可用于治疗乙醇使用障碍戒断，焦虑和/或抑郁，精神分裂症，躁狂症或创伤后应激障碍的选择性κ阿片受体效应物或其药学上可接受的盐。

公开(公告)号：US09540375B2

公开(公告)日：2017-01-10

申请号：US15156887

申请日：2016-05-17

申请人： University of Kansas ,  The Scripps Research Institute

发明人： Jeffrey Aube ,  Laura Bohn ,  Thomas Edward Prisinzano ,  Frank John Schoenen ,  Kevin J. Frankowski

IPC分类号： C07D403/14 ,  C07D249/12 ,  C07D471/14 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4985 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D471/14 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4985 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.

摘要翻译： 本发明是可用于治疗乙醇使用障碍戒断，焦虑和/或抑郁，精神分裂症，躁狂症或创伤后应激障碍的选择性κ阿片受体效应物或其药学上可接受的盐。

公开(公告)号：US09464035B2

公开(公告)日：2016-10-11

申请号：US14388494

申请日：2013-03-15

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Services ,  The University of Kansas

发明人： Juan Jose Marugan ,  Wei Zheng ,  Samarjit Patnaik ,  Noel Southall ,  Ellen Sidransky ,  Ehud Goldin ,  Wendy Westbroek ,  Elma Aflaki ,  Steven Andrew Rogers ,  Frank John Schoenen

IPC分类号： C07C235/64 ,  C07C235/60 ,  C07C237/22

CPC分类号： C07C235/64 ,  C07B2200/07 ,  C07C235/60 ,  C07C237/22

摘要： Compounds of Formula (I) and the pharmaceutically acceptable salts thereof are disclosed. The variables. R1-R13, m, n, o, and p are disclosed herein. The compounds are useful for treating Gaucher disease and inhibiting the onset of Gaucher disease symptoms in a patient having a GBA gene mutation and for treating Parkinson's disease. Pharmaceutical compositions containing compounds of Formula (I) and methods of treatment comprising administering compounds of Formula (I) are also disclosed.

公开(公告)号：US20240342179A1

公开(公告)日：2024-10-17

申请号：US18635508

申请日：2024-04-15

申请人： University of Kansas

发明人： Andrew K. Godwin ,  Frank John Schoenen ,  Anuradha Roy ,  Benjamin Gibbs ,  Rebecca Wates

IPC分类号： A61K31/519 ,  A61K31/198 ,  A61K31/433 ,  A61K31/4436 ,  A61K31/506 ,  A61K31/517 ,  A61K38/17 ,  A61P35/00 ,  C12N15/113

CPC分类号： A61K31/519 ,  A61K31/198 ,  A61K31/433 ,  A61K31/4436 ,  A61K31/506 ,  A61K31/517 ,  A61K38/1709 ,  A61P35/00 ,  C12N15/113 ,  C12N2310/14

摘要： A method of inhibiting KIF15 can include administering a compound to the KIF15 to inhibit biological functionality of KIF15. The compound includes a structure of Formula 1. R1 and R2 are each independently a non-hydrogen substituent, such that the compound inhibits biological functionality of KIF15, or a stereoisomeric form or a mixture of stereoisomeric forms, or pharmaceutically acceptable salts of the compound. The compound is administered to the KIF15 to inhibit KIF15 from interacting with TPX2 so as to inhibit or disrupt a protein-protein interaction therebetween. The administering of the compound can be to a subject having the KIF15, which is administered in a therapeutically effective amount to treat a disease or disorder associated with KIF15 interacting with TPX2, such as treating a cancer or neoplasm.

公开(公告)号：US20150322087A1

公开(公告)日：2015-11-12

申请号：US14439373

申请日：2013-11-04

申请人： UNIVERSITY OF KANSAS ,  CORNELL UNIVERSITY

发明人： Jeffrey Aube ,  Carl Nathan ,  Robert Smith ,  Ben S. Gold ,  Paul Hanson ,  Chunjing Liu ,  Lester Allen Mitscher ,  Maneesh Pingle ,  Frank John Schoenen

IPC分类号： C07D501/16 ,  A61K31/43 ,  C07D277/06 ,  A61K31/426 ,  A61K45/06 ,  A61K31/427 ,  C07D513/04 ,  A61K31/429 ,  A61K31/545 ,  A61K31/546 ,  C07D499/44 ,  C07D417/12

CPC分类号： C07D501/16 ,  A61K31/426 ,  A61K31/427 ,  A61K31/429 ,  A61K31/43 ,  A61K31/431 ,  A61K31/4725 ,  A61K31/545 ,  A61K31/546 ,  A61K45/06 ,  C07D277/06 ,  C07D417/12 ,  C07D499/44 ,  C07D513/04 ,  Y02A50/401 ,  Y02A50/402 ,  A61K2300/00

摘要： This invention provides cephalosporin derivatives for killing or inhibiting the spread of microorganisms such as non-replicating Mycobacterium tuberculosis and in the treatment of infectious disease.

摘要翻译： 本发明提供头孢菌素衍生物用于杀死或抑制微生物如非复制型结核分枝杆菌的扩散和用于治疗感染性疾病。

公开(公告)号：US10059722B2

公开(公告)日：2018-08-28

申请号：US14439373

申请日：2013-11-04

申请人： University of Kansas ,  Cornell University

发明人： Jeffrey Aube ,  Carl Nathan ,  Robert Smith ,  Ben S. Gold ,  Paul Hanson ,  Chunjing Liu ,  Lester Allen Mitscher ,  Maneesh Pingle ,  Frank John Schoenen

IPC分类号： C07D501/60 ,  C07D501/16 ,  A61K31/545 ,  C07D499/44 ,  C07D277/06 ,  C07D417/12 ,  C07D513/04 ,  A61K45/06 ,  A61K31/426 ,  A61K31/427 ,  A61K31/429 ,  A61K31/43 ,  A61K31/431 ,  A61K31/4725 ,  A61K31/546

CPC分类号： C07D501/16 ,  A61K31/426 ,  A61K31/427 ,  A61K31/429 ,  A61K31/43 ,  A61K31/431 ,  A61K31/4725 ,  A61K31/545 ,  A61K31/546 ,  A61K45/06 ,  C07D277/06 ,  C07D417/12 ,  C07D499/44 ,  C07D513/04 ,  Y02A50/401 ,  Y02A50/402 ,  A61K2300/00

摘要： This invention provides cephalosporin derivatives for killing or inhibiting the spread of microorganisms such as non-replicating Mycobacterium tuberculosis and in the treatment of infectious disease.

公开(公告)号：US20150065469A1

公开(公告)日：2015-03-05

申请号：US14388494

申请日：2013-03-15

申请人： The USA, as Represented by the Secretary, Department of Health and Human Services ,  The University of Kansas

发明人： Juan Jose Marugan ,  Wei Zheng ,  Samarjit Patnaik ,  Noel Southall ,  Ellen Sidransky ,  Ehud Goldin ,  Wendy Westbroek ,  Elma Aflaki ,  Steven Andrew Rogers ,  Frank John Schoenen

IPC分类号： C07C235/64

CPC分类号： C07C235/64 ,  C07B2200/07 ,  C07C235/60 ,  C07C237/22

摘要： Compounds of Formula (I) and the pharmaceutically acceptable salts thereof are disclosed. The variables. R1-R13, m, n, o, and p are disclosed herein. The compounds are useful for treating Gaucher disease and inhibiting the onset of Gaucher disease symptoms in a patient having a GBA gene mutation and for treating Parkinson's disease. Pharmaceutical compositions containing compounds of Formula (I) and methods of treatment comprising administering compounds of Formula (I) are also disclosed.

摘要翻译： 公开了式（I）化合物及其药学上可接受的盐。 变量。 本文公开了R1-R13，m，n，o和p。 该化合物可用于治疗戈谢病并抑制具有GBA基因突变的患者和治疗帕金森病的戈谢病症状发作。 还公开了含有式（I）化合物和包括施用式（I）化合物的治疗方法的药物组合物。

公开(公告)号：US09745261B2

公开(公告)日：2017-08-29

申请号：US14897445

申请日：2014-06-10

申请人： THE GENERAL HOSPITAL CORPORATION ,  THE BROAD INSTITUTE, INC. ,  UNIVERSITY OF KANSAS

发明人： Patrick Faloon ,  Warren S. Weiner ,  Robert A. Smith ,  Frank John Schoenen ,  David E. Fisher ,  Rizwan Haq

IPC分类号： C07C311/16 ,  A61K31/18 ,  C07C311/17 ,  C07D333/34 ,  C07D409/12 ,  C07D209/48 ,  C07D307/91 ,  C07D307/68 ,  A61K31/4184

CPC分类号： C07C311/17 ,  A61K31/4184 ,  C07D209/48 ,  C07D307/68 ,  C07D307/91 ,  C07D333/34 ,  C07D409/12

摘要： Provided herein are compounds of the formula (IV) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful as MITF inhibitors, MITF pathway inhibitors and for the treatment of cancer.